LY 333531 hydrochloride

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Cat.No. 4738 - LY 333531 hydrochloride | C28H28N4O3.HCl | CAS No. 169939-93-9
Description: Protein kinase C inhibitor; selective for β isozymes
Alternative Names: Ruboxistaurin
Chemical Name: (9S)-9-[(Dimethylamino)methyl]-6,7,10,11-tetrahydro-9H,18H-5,21:12,17-dimethenodibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecine-18,20(19H)-dione hydrochloride
Datasheet
Citations (2)
Reviews
Literature

Biological Activity

Isozyme-selective inhibitor of protein kinase C (PKC); competitively and reversibly inhibits PKCβI and PKCβII (IC50 values are 4.7 and 5.9 nM respectively). Selective for PKCβ over other PKC isozymes (IC50 values are 0.052, 0.25, 0.30, 0.36, 0.60 and >100 μM for PKCη, -δ, -γ, -α, -ε and -ζ respectively). Exhibits selectivity for PKC over other ATP-dependent kinases, including protein kinase A, casein kinase and src).

Technical Data

M. Wt 505.01
Formula C28H28N4O3.HCl
Storage Store at -20°C
CAS Number 169939-93-9
PubChem ID 9870785
InChI Key NYQIEYDJYFVLPO-FERBBOLQSA-N
Smiles O=C(C(C4=CN(CCO[C@H](CN(C)C)CC6)C5=C4C=CC=C5)=C1C2=CN6C3=CC=CC=C23)NC1=O.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 10.1 20

Preparing Stock Solutions

The following data is based on the product molecular weight 505.01. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.2 mM 9.9 mL 49.5 mL 99.01 mL
1 mM 1.98 mL 9.9 mL 19.8 mL
2 mM 0.99 mL 4.95 mL 9.9 mL
10 mM 0.2 mL 0.99 mL 1.98 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

References are publications that support the biological activity of the product.

Jirousek et al (1996) (S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16,21-dimetheno-1H,13H-dibenzo[e,k]]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-dione (LY333531) and related analogues: isozyme selec J.Med.Chem. 39 2664 PMID: 8709095

Faul et al (2003) Acyclic N-(azacycloalkyl)bisindolylmaleimides: isozyme selective inhibitors of PKCβ. Bioorg.Med.Chem.Lett. 13 1857 PMID: 12749884

Samokhin et al (1999) Effects of protein kinase C inhibitors on thromboxane production by thrombin-stimulated platelets. Eur.J.Pharmacol. 386 297 PMID: 10618482

Lewin et al (2018) Synthesis and Characterization of the Selective, Reversible PKC beta Inhibitor (9S)-9-[(Dimethylamino)methyl]-6,7,10,11-tetrahydro-9H,18H-5,21:12,17-dimethenodibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecine-18,20(19H)-dione, Ruboxistaurin (LY333531) A.C.S.Chem.Neurosci.


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2 Citations for LY 333531 hydrochloride

Citations are publications that use Tocris products. Selected citations for LY 333531 hydrochloride include:

Cosgrove (2016) N-cadherin adhesive interactions modulate matrix mechanosensing and fate commitment of mesenchymal stem cells. Nature Materials 15 1297 PMID: 27525568

Muellner et al (2015) Targeting a cell state common to triple-negative breast cancers. ASN Neuro 11 789 PMID: 25699542


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